| Description | Hu7691 is an orally active, selective and potent Akt inhibitor that inhibits Akt1, Akt2 and Akt3, inhibits proliferation of neuroblastoma cells and induces differentiation of neuroblastoma cells. |
| In vitro | Hu7691 对多种神经母细胞瘤细胞系的抗增殖和神经发生作用。包括神经突出生长、细胞周期阻滞以及分化mRNA标记物，进一步阐明了 Hu7691 的诱导分化效果[3]。 |
| In vivo | 对于 Hu7691 在雄性和雌性 Sprague Dawley (SD) 大鼠中进行连续14天反复剂量毒性研究，结果表明：雄性大鼠每天接受12.5、50、100和150 mg/kg的剂量，而雌性大鼠连续14天每天接受12.5、25、50和75 mg/kg 的剂量。毒性评估表明潜在的毒性靶器官包括脾脏、胸腺和胃肠道[2]。 |
| Target activity | Akt3:28 nM, RSK1:756 nM, ROCK1:354 nM, PKCη:629 nM, p70 S6K:229 nM, PKA:11 nM, Akt2:97.5 nM, Akt1:4.0 nM |
| molecular weight | 450.88 |
| Molecular formula | C22H22ClF3N4O |
| CAS | 2360523-76-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL(229.00 mM), Sonication is recommended. |
| References | 1. Junya Kawai, et al. Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold. ACS Med Chem Lett. 2019 May 24;10(6):893-898. 2. Gai R, Chen C, Zhang W, Ma J, Wang X, Chi X, Li G. Safety and Toxicology Study of Hu7691, a Novel AKT Inhibitor, following Oral Administration in Rats. Toxics. 2023 Oct 26;11(11):880. 3. Bing S,et al. AKT inhibitor Hu7691 induces differentiation of neuroblastoma cells. Acta Pharm Sin B. 2023 Apr;13(4):1522-1536. |